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171179-06-9

中文名称 N4-(3-溴苯基)-N6-甲基-吡啶并[3,4-D]嘧啶-4,6-二胺
英文名称 PD158780
CAS 171179-06-9
分子式 C14H12BrN5
分子量 330.188
MOL 文件 171179-06-9.mol
更新日期 2024/07/15 17:11:00
171179-06-9 结构式 171179-06-9 结构式

基本信息

中文别名
化合物PD158780
N4-(3-溴苯基)-N6-甲基-吡啶并[3,4-D]嘧啶-4,6-二胺
英文别名
PD 158780 solution
PD 158780
PD-158780
InSolution? PD 158780
PD 158780 - CAS 171179-06-9 - Calbiochem
InSolution PD 158780 - CAS 171179-06-9 - Calbiochem
N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine
Pyrido[3,4-d]pyriMidine-4,6-diaMine,N4-(3-broMophenyl)-N6-Methyl-
Pyrido[3,4-d]pyriMidine-4,6-diaMine,N4-(3-broMophenyl)-N6-Methyl- (Related Reference)

物理化学性质

熔点174.0 to 178.0 °C
沸点499.6±45.0 °C(Predicted)
密度1.611±0.06 g/cm3 (20 ºC 760 Torr)
储存条件-20°C储存
储存条件Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度二甲基亚砜:≥20mg/mL
酸度系数(pKa)5.80±0.30(Predicted)
形态黄色固体
颜色黄色

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302
危险品标志Xn
危险类别码22
海关编码2912.49.2600
N4-(3-溴苯基)-N6-甲基-吡啶并[3,4-D]嘧啶-4,6-二胺价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30P2567PD 158780
PD 158780
171179-06-910mg420元
2024/04/30P2567PD 158780
PD 158780
171179-06-950mg1730元

常见问题列表

生物活性
PD158780是有效地 EGFR 家族抑制剂;对EGFR,ErbB2,ErbB3和ErbB4的 IC50 值分别为8 μM,49,52,52 nM。
靶点

EGFR

8 μM (IC 50 , Cell Assay)

ErbB2

49 nM (IC 50 , Cell Assay)

ErbB3

52 nM (IC 50 , Cell Assay)

ErbB4

52 nM (IC 50 , Cell Assay)

体外研究

PD158780 inhibits EGF receptor autophosphorylation in A431 human epidermoid carcinoma with IC 50 value of 13 nM. PD158780 is highly specific for the EGF receptor in Swiss 3T3 fibroblasts, inhibiting EGF-dependent receptor autophosphorylation and thymidine incorporation at low nanomolar concentrations while requiring micromolar levels for platelet-derived growth factor- and basic fibroblast growth factordependent processes. PD158780 inhibits heregulin-stimulated phosphorylation in the SK-BR-3 and MDAMB-453 breast carcinomas with IC 50 values of 49 and 52 nM, respectively, suggesting that the compound is active against other members of the EGF receptor family.

体内研究

PD158780 is active against clone formation in several breast tumors having different expression patterns of the ErbB family. PD158780 shows good therapeutic effect against the A431 epidermoid carcinoma when administered either intraperitoneally or orally. PD158780 produces measurable, significant effects against a mouse fibroblast transfected with human EGFR. PD158780 produces a significant therapeutic effect against the estrogendependent MCF-7 breast carcinoma at equitoxic dose levels.

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